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In this scenario the receptor
2023-08-11

In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; P 95% CI: 0.6
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ATP citrate lyase ACLY is a
2023-08-11

ATP citrate lyase (ACLY) is a cytosolic enzyme that catalyzes the generation of acetyl-CoA from citrate [15]. Acetyl-CoA is the building block for the biosynthesis of fatty acids and cholesterol, and also serves as a substrate of the acetylation reaction of various molecules, including histones and
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On the other hand there
2023-08-11

On the other hand, there were only a few cases that expressed DA2R in our study. Additionally, in the cases whose ACTH-secreting pituitary adenomas expressed DA2R, the ratio of positive staining LY3009104 was very low. This suggests that dopamine agonists may be less effective in canine Cushing's d
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It is well known that neurosteroids such as testosterone
2023-08-11

It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls
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NOS is classified into three isoforms endothelial
2023-08-11

NOS is classified into three isoforms: endothelial (eNOS), neuronal (nNOS), and inducible (iNOS), iNOS is expressed in macrophages (Eisenstein, Huang, Meissler Jr, & al-Ramadi, 1994) and osteoblast-like cells (Riancho et al., 1995) and is involved in the regulation of inflammatory reactions (Eisenst
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Methods We conducted a secondary analysis
2023-08-11

Methods We conducted a secondary analysis of an extant cohort of 580 infants hylaxis, premature rupture of membranes, chorioamnionitis, and to prolong pregnancy (latency). Maternal antibiotic exposure did not include RJR-2403 oxalate given after the time of delivery or antibiotic initiated by surg
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br Concluding Remarks and Future Perspectives The collective
2023-08-11

Concluding Remarks and Future Perspectives The collective evidence from studies detailing the functions of AMPK in the neuromuscular system, combined with those in DMD, SMA, and DM1 surveyed in the present review, strongly suggests that AMPK is a central mediator of neuromuscular determination, m
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br Results The newly synthesized
2023-08-11

Results The newly synthesized leucine ureido derivatives were firstly evaluated for their enzymatic inhibition using porcine kidney APN (Microsomal, Biocol) with bestatin as the positive control (Table 1). One isoleucine ureido derivative 14 and phenylglycine ureido derivative 15 were also synthe
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To guide our attempts at achieving
2023-08-11

To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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The present study determined the effect
2023-08-11

The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that 2-NBDG non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular calcificatio
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br Materials and methods br Results br
2023-08-11

Materials and methods Results Discussion Conclusions These studies provide important mechanistic insights to explain the long-established physiological observation that obese adipose tissue has higher rates of basal lipolysis. Increased lipolysis contributes to increased hepatic DC_AC50
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HT receptors are distributed throughout the brain within
2023-08-11

5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and E3330 (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Bufton et al., 19
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The same applies also to intermediate formally obtained by e
2023-08-11

The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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During the course of our ACK inhibitor program a high
2023-08-11

During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of identif
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Based on the improved characteristics of
2023-08-11

Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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